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Pharm 845 Exam #3 > Muscle Relaxants & Ethanol- Dr. Masserano > Flashcards

Muscle Relaxants & Ethanol- Dr. Masserano Flashcards

1
Q

Examples of acute muscle spasm

A

-Lower back pain
-Neck pain
-Tension headache
-TMJ
(Treat with Antispasmodic drugs)

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2
Q

Examples of chronic conditions

A

-Cerebral palsy
-Multiple sclerosis
-Spinal cord injury
-Stroke
-Fibromyalgia
-Myofascial pain syndrom
(Treat with antispasticity drugs)

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3
Q

When to use antispasmodic agents

A

-Musculoskeletal conditions

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4
Q

When to use antispasticity agents

A

-Upper motor neuron disorders

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5
Q

List some antispasmodic agents

A
  • Cyclobenzaprine
  • Methocarbamol
  • Carisoprodol
  • Chlorzoxazone
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6
Q

List some anti spastic agents

A
  • Baclofen (safe in elderly)

- Dantrolene

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7
Q

Which two agents have both antispastic and antispasmodic properties

A
  • Diazepam

- Tizanidine (safe in elderly)

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8
Q

What are 1st, 2nd, and 3rd line treatment options for both acute and chronic lower back pain

A 
Acute pain
-1st line: Tylenol/NSAIDs
-2nd line: Skeletal muscle relaxants
-3rd line: Opioids
Chronic pain 
-1st line: Tylenol/ NSAIDs
-2nd line: TCAs/SNRIs
-3rd line: Skeletal muscle relaxants/ opioids
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9
Q

Diazepam (Valium) MoA

A
  • Potentiates GABA hyperpolarization (Cl- channel) by action on the GABAa receptor
  • Site of action: CNS and Spinal cord
  • Treats antispasticity and antispasmodic disorders
  • Sedation: Main side effect
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10
Q

Baclofen (Lioresal)

A
  • Derivative of GABAb
  • Decreases calcium influx and transmitter release (decreasing glutamate)
  • Increases K+ efflux (Hyperpolarizing)
  • Recommended for treatment of spasticity
  • Do NOT abruptly DC, gradually reduce the dose
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11
Q

Tizanidine (Zanaflex)

A
  • Alpha 2 agonist
  • Decreases calcium flow into presynaptic neuron
  • Decreasing glutamate release
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12
Q

Dantrolene (Dantrium)

A
  • Inhibits RyR1 channel in skeletal muscle
  • Inhibits calcium release intracellularly
  • Thus inhibiting contractions
  • Treatment for spasticity
  • Also can treat malignant hyperthermia
  • No effect on cardiac/smooth muscle (RyR2 is found here)
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13
Q

Black box warning with Dantrolene (Dantrium)

A
  • Discontinue if no benefit with in 45 days

- Potential for hepatotoxicity

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14
Q

What do alpha 2 agonists do

A
  • Decrease Ca++ uptake

- Decreasing glutamate release

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15
Q

Cyclobenzaprine (Flexril, Amrox) MoA

A
  • Works on upper CNS
  • Alpha 2 agonist
  • 5HT2 antagonist
  • May prolong QT interval
  • Potential for serotonin syndrome (when combined with TCAs, SSRIs, SNRIs, MAOIs)
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16
Q

Carisoprodol (Soma) MoA and drug schedule

A
  • Schedule IV
  • Do not combine with other CNS depressants
  • Potential for drug abuse, dependence, and withdrawal
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17
Q

Methocarbamol (Robaxin) MoA

A
  • CNS depressant
  • Treats acute musculoskeletal pain
  • Can cause sedation
18
Q

Palcohol

A
  • Freeze dried alcohol
  • Federally legal
  • Illegal in many states
  • Exceptions: NM and CO
19
Q

CNS depression increases with more or less hydrocarbons?

A
  • Increase hydrocarbons = increased CNS depression

- Isopropanol > Ethanol> Methanol

20
Q

Who will have a higher blood alcohol level; an obese patient or an healthy patient

A
  • The obese patient
  • Distributed though water
  • Increased fat content = decreased water content
21
Q

What is the value of “r” in men vs women

A
  • Men = 0.68

- Women = 0.55

22
Q

How many grams of ethanol is in one standard drink?

A

-14.4 grams

23
Q

What type of kinetics does ETOH follow?

A
  • Zero order kinetics

- One drink takes about 1.5 to 2hrs to be eliminated

24
Q

What enzymes are involved in the metabolism of ETOH

A
  • Alcohol dehydrogenase

- Aldehyde dehydrogenase

25
Q

Why are asians light weights?

A
  • Higher Km for aldehyde (lower activity)
  • Making them slower metabolizers
  • Build up of aldehyde levels lead to poor side effects
  • Deters these people from drinking
26
Q

What are some effects of ETOH on the body

A
  • Lactate acidosis
  • Hyperlipidemia
  • Severe liver damage
  • Hypoglycemia
27
Q

What is the use of fructose in alcohol overdose

A
  • May help to rapidly reoxidize NADH to NAD
  • Increasing the metabolism of alcohols metabolites
  • Can increase the metabolism by up to 20%
28
Q

CNS effects of ETOH

A
  • Sedation
  • Anticonvulsant
  • Analgesic
  • Sleep effects
29
Q

Total body effects of chronic ETOH ingestion

A
  • Liver damage
  • GI tract issues
  • Muscle damage
  • Heart/CV effects
  • Kidney
  • CNS
30
Q

Positive effects of ETOH use in MODERATION

A
  • Decreases CV risk
  • Improves lipid profile
  • Makes blood vessels healthier
  • Decreases BP
  • Decreases inflammation
31
Q

Wernicke-Korsakoff syndrome

A 
-Due to malabsorption of thiamine (B1)
Wernicke's disease:
-Opthalmic difficulties
-Ataxia of gait
-Disoriented
Treatment: supplement with B1
32
Q

How do you treat methanol and ethylene glycol poisoning

A

-Competitively block alcohol dehydrogenase

33
Q

What is Denatonium Benzoate

A
  • Additive to antifreeze

- Makes it taste bitter so your dog wont eat it

34
Q

MoA of Fomepizole (Antizol)

A
  • Injection that competitively inhibits alcohol dehydrogenase
  • Used in treatment of methanol/ethylene glycol poisoning
  • Used in combo with hemodialysis and general supportive care
35
Q

Acute drug ints with ETOH

A

Increases the half life of:

  • Warfarin
  • Tylenol
36
Q

Drug ints with chronic ETOH

A
  • Decreases half life of Tylenol

- Increases toxic quinone when ETOH leaves system

37
Q

Tylenol and ETOH better explained

A
  • Tylenol is metabolized by CYP2E1 to a toxic quinone
  • Ethanol competes with Tylenol (induces CYP2E1)
  • Once ETOH is eliminated the production of toxic quinone is increased (due to upregulation of CYP2E1)
38
Q

Disulfiram (Antabuse)

A

-Blocks the conversion of acetaldehyde to acetic acid by inhibiting aldehyde dehydrogenase

39
Q

Naltrexone (Revia)

A
  • Long acting opioid antagonist
  • Helps to reduce relapse rates in alcoholics
  • Diminishes the “high” of ETOH
40
Q

Acamprosate (Campral)

A
  • Blocks glutamatergic N methyl D asparte receptors
  • While activating GABAb receptors
  • Must be abstinent from ETOH at the initiation of treatment
41
Q

Varenicline (Chantix)

A
  • Helps to reduce alcohol consumption and alcohol cravings

- Best for pts that are also trying to quit smoking

Pharm 845 Exam #3 (7 decks)

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